Wise R, Webberley J M, Andrews J M, Ashby J P
Department of Medical Microbiology, Dudley Road Hospital, Birmingham, UK.
J Antimicrob Chemother. 1988 Jan;21(1):85-91. doi: 10.1093/jac/21.1.85.
The pharmacokinetics of CGP 31608, a new injectable penem antibiotic, were studied following a 1 g intravenous infusion. Concentrations were determined in serum, urine and cantharidin-induced inflammatory fluid by a microbiological assay. Peak serum concentrations were achieved at, or before the end of, the 1 h infusion, with a mean of 24.9 mg/l occurring at 0.8 h. The mean serum elimination half-life was 0.5 h, with no detectable drug in serum after 3 h. Inflammatory fluid was penetrated rapidly with a mean peak level of 10.5 mg/l occurring at 1.3 h (i.e. 20 min after the end of the infusion). Urinary elimination of CGP 31608 accounted for 52.1% of the administered dose within an hour of finishing the infusion, and 57.1% by 12 h. This study suggests that therapeutic serum levels (greater than 8 mg/l) are present for about 1.5 h after starting a 1 h infusion, and in inflammatory fluid for about 2.5 h. Unless a dose in excess of 1 g is used, CGP 31608 will probably have to be given four or more times a day.
对新型注射用青霉烯类抗生素CGP 31608进行1克静脉输注后，研究了其药代动力学。通过微生物学测定法测定血清、尿液和斑蝥素诱导的炎性渗出液中的浓度。在1小时输注结束时或之前达到血清峰值浓度，0.8小时时的平均浓度为24.9毫克/升。血清消除半衰期的平均值为0.5小时，3小时后血清中未检测到药物。炎性渗出液迅速被渗透，1.3小时（即输注结束后20分钟）时的平均峰值水平为10.5毫克/升。输注结束后1小时内，CGP 31608经尿液消除的量占给药剂量的52.1%，12小时时占57.1%。本研究表明，开始1小时输注后约1.5小时血清中存在治疗水平（大于8毫克/升），在炎性渗出液中约2.5小时。除非使用超过1克的剂量，否则CGP 31608可能每天需要给药四次或更多次。
